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Assay Detail

CHEMBL4815473

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL ↗
51
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL3759) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H<sub>2</sub>R and D<sub>3</sub>R.
Biselli S, Bresinsky M, Tropmann K, Forster L, Honisch C, Buschauer A, Bernhardt G, Pockes S.
Eur J Med Chem (2021) 214 : 113190 -113190
PubMed 33548637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 4.93 7.60
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90 HISTAMINE 4.0 1 7.60
CHEMBL4846201 — — 1 6.11
CHEMBL4846638 — — 1 5.72
CHEMBL4871482 — — 1 5.58
CHEMBL4865765 — — 1 5.49
CHEMBL4853107 — — 1 5.44
CHEMBL4857560 — — 1 5.43
CHEMBL4860528 — — 1 5.37
CHEMBL4866734 — — 1 5.31
CHEMBL4856572 — — 1 5.23
CHEMBL4876025 — — 1 5.20
CHEMBL4848815 — — 1 5.17
CHEMBL4858849 — — 1 5.10
CHEMBL4853668 — — 1 5.09
CHEMBL4863523 — — 1 5.09
CHEMBL4876267 — — 1 5.09
CHEMBL4863347 — — 1 5.07
CHEMBL4872375 — — 1 5.02
CHEMBL4869194 — — 1 4.95
CHEMBL4870510 — — 1 4.95
CHEMBL4852212 — — 1 4.92
CHEMBL4864852 — — 1 4.89
CHEMBL4875600 — — 1 4.88
CHEMBL4856059 — — 1 4.87
CHEMBL4874969 — — 1 4.87
CHEMBL4869389 — — 1 4.87
CHEMBL4848697 — — 1 4.86
CHEMBL4864067 — — 1 4.83
CHEMBL4876799 — — 1 4.78
CHEMBL4850448 — — 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90 HISTAMINE Ki = 25.12 nM 7.60
CHEMBL4846201 — Ki = 776.25 nM 6.11
CHEMBL4846638 — Ki = 1905.46 nM 5.72
CHEMBL4871482 — Ki = 2630.27 nM 5.58
CHEMBL4865765 — Ki = 3235.94 nM 5.49
CHEMBL4853107 — Ki = 3630.78 nM 5.44
CHEMBL4857560 — Ki = 3715.35 nM 5.43
CHEMBL4860528 — Ki = 4265.8 nM 5.37
CHEMBL4866734 — Ki = 4897.79 nM 5.31
CHEMBL4856572 — Ki = 5888.44 nM 5.23
CHEMBL4876025 — Ki = 6309.57 nM 5.20
CHEMBL4848815 — Ki = 6760.83 nM 5.17
CHEMBL4858849 — Ki = 7943.28 nM 5.10
CHEMBL4876267 — Ki = 8128.31 nM 5.09
CHEMBL4853668 — Ki = 8128.31 nM 5.09
CHEMBL4863523 — Ki = 8128.31 nM 5.09
CHEMBL4863347 — Ki = 8511.38 nM 5.07
CHEMBL4872375 — Ki = 9549.93 nM 5.02
CHEMBL4869194 — Ki = 11220.18 nM 4.95
CHEMBL4870510 — Ki = 11220.18 nM 4.95
CHEMBL4852212 — Ki = 12022.64 nM 4.92
CHEMBL4864852 — Ki = 12882.5 nM 4.89
CHEMBL4875600 — Ki = 13182.57 nM 4.88
CHEMBL4869389 — Ki = 13489.63 nM 4.87
CHEMBL4856059 — Ki = 13489.63 nM 4.87
CHEMBL4874969 — Ki = 13489.63 nM 4.87
CHEMBL4848697 — Ki = 13803.84 nM 4.86
CHEMBL4864067 — Ki = 14791.08 nM 4.83
CHEMBL4876799 — Ki = 16595.87 nM 4.78
CHEMBL4850448 — Ki = 17378.01 nM 4.76
CHEMBL4867962 — Ki = 17782.79 nM 4.75
CHEMBL4856005 — Ki = 19054.61 nM 4.72
CHEMBL4848026 — Ki = 19952.62 nM 4.70
CHEMBL4856200 — Ki = 21379.62 nM 4.67
CHEMBL4858567 — Ki = 22387.21 nM 4.65
CHEMBL4856602 — Ki = 23442.29 nM 4.63
CHEMBL4853772 — Ki = 26915.35 nM 4.57
CHEMBL4871221 — Ki = 30199.52 nM 4.52
CHEMBL4861704 — Ki = 30199.52 nM 4.52
CHEMBL4878215 — Ki = 30199.52 nM 4.52
CHEMBL4876743 — Ki = 31622.78 nM 4.50
CHEMBL4845733 — Ki = 32359.37 nM 4.49
CHEMBL4872277 — Ki = 34673.69 nM 4.46
CHEMBL4850490 — Ki = 44668.36 nM 4.35
CHEMBL4846380 — Ki = 45708.82 nM 4.34
CHEMBL4854278 — Ki = 54954.09 nM 4.26
CHEMBL4863393 — Ki = 64565.42 nM 4.19
CHEMBL4865965 — Ki = 75857.76 nM 4.12
CHEMBL4874758 — Ki = 87096.36 nM 4.06
CHEMBL4865670 — Ki > 100000.0 nM -